Publication Date:
1996-08-09
Description:
alpha2-Adrenergic receptors (alpha2ARs) present in the brainstem decrease blood pressure and are targets for clinically effective antihypertensive drugs. The existence of three alpha2AR subtypes, the lack of subtype-specific ligands, and the cross-reactivity of alpha2AR agonists with imidazoline receptors has precluded an understanding of the role of individual alpha2AR subtypes in the hypotensive response. Gene targeting was used to introduce a point mutation into the alpha2aAR subtype in the mouse genome. The hypotensive response to alpha2AR agonists was lost in the mutant mice, demonstrating that the alpha2aAR subtype plays a principal role in this response.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉MacMillan, L B -- Hein, L -- Smith, M S -- Piascik, M T -- Limbird, L E -- HL38120/HL/NHLBI NIH HHS/ -- HL43671/HL/NHLBI NIH HHS/ -- HL48638/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1996 Aug 9;273(5276):801-3.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/8670421" target="_blank"〉PubMed〈/a〉
Keywords:
Adrenergic alpha-2 Receptor Agonists
;
Adrenergic alpha-Agonists/pharmacology
;
Animals
;
Antihypertensive Agents/pharmacology
;
Base Sequence
;
Blood Pressure/drug effects/*physiology
;
Brain Stem/physiology
;
Brimonidine Tartrate
;
Gene Targeting
;
Heart Rate/drug effects/physiology
;
Imidazoles/pharmacology
;
Medetomidine
;
Mice
;
Mice, Inbred C57BL
;
Molecular Sequence Data
;
Point Mutation
;
Quinoxalines/pharmacology
;
Receptors, Adrenergic, alpha-2/genetics/metabolism/*physiology
Print ISSN:
0036-8075
Electronic ISSN:
1095-9203
Topics:
Biology
,
Chemistry and Pharmacology
,
Computer Science
,
Medicine
,
Natural Sciences in General
,
Physics
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